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Chemical Structure : E6201
Catalog No.: PC-62503Not For Human Use, Lab Use Only.
E 6201 (ER-806201) is a potent, selective, dual MEK1 and MEKK1 inhibitor, inhibits LPS-induced TNFα transcription with IC50 of 50 nM.
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E 6201 (ER-806201) is a potent, selective, dual MEK1 and MEKK1 inhibitor, inhibits LPS-induced TNFα transcription with IC50 of 50 nM.
E 6201 does not suppress β-actin transcription at 3 uM and only slightly at 10 uM.
E 6201 inhibits MEK1-induced ERK2 phosphorylation with IC50 of 5.2 nM, MKK4-induced JNK phosphorylation with IC50 of 91 nM, and MKK6-induced p38α MAPK phosphorylation with IC50 of 19 nM.
E 6201 also inhibits MEKK1-induced phosphorylation of MEK1, MKK4, and MKK6 with IC50 of 31, 522, and 65 nM, respectively, has no effect on other MAPK family enzymes such as ERK2, JNKs, and p38 MAPK at 10 uM.E 6201 inhibits TNFα, IL-1β, IL-6, and IL-8 production from LPS-stimulated human PBMCs.
| M.Wt | 389.44 | |
| Formula | C21H27NO6 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Goto M, et al. J Pharmacol Exp Ther. 2009 Nov;331(2):485-95.
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